Dolfen Daniel, Schottler Kristina, Valiahdi Seied-Mojtaba, Jakupec Michael A, Keppler Bernhard K, Tiekink Edward R T, Mohr Fabian
Fachbereich C, Anorganische Chemie, Bergische Universität Wuppertal, 42119 Wuppertal, Germany.
J Inorg Biochem. 2008 Dec;102(12):2067-71. doi: 10.1016/j.jinorgbio.2008.07.002. Epub 2008 Jul 11.
The thiocarbamate esters 4-RC6H4NHC(S)OMe (R = H, Cl, OMe, NO2, Me) react with cis-[PtCl2(PTA)2] (PTA=1,3,5-triaza-7-phosphaadamantane) in the presence of base to afford the platinum(II) complexes trans-[Pt{SC(OMe)NC6H4R}2(PTA)2] (R=H, Cl, OMe, NO2, Me) in high yields. The complexes were fully characterised spectroscopically and, in case of the NO2 derivate, by X-ray crystallography. Cytotoxicity of these complexes was studied in vitro in four human cancer cell lines (CH1, HT29, A549, SK-OV-3) using the MTT assay. The results show that the Cl substituted derivate is the most potent of these compounds in vitro. Moreover, this derivative is capable of partially circumventing primary cisplatin resistance in ovarian and colon carcinoma cells.
硫代氨基甲酸酯4-RC6H4NHC(S)OMe(R = H、Cl、OMe、NO2、Me)在碱存在下与顺式-[PtCl2(PTA)2](PTA = 1,3,5-三氮杂-7-磷杂金刚烷)反应,高产率地得到铂(II)配合物反式-[Pt{SC(OMe)NC6H4R}2(PTA)2](R = H、Cl、OMe、NO2、Me)。通过光谱对这些配合物进行了全面表征,对于NO2衍生物,还通过X射线晶体学进行了表征。使用MTT法在四种人癌细胞系(CH1、HT29、A549、SK-OV-3)中体外研究了这些配合物的细胞毒性。结果表明,Cl取代的衍生物在体外是这些化合物中最有效的。此外,该衍生物能够部分克服卵巢癌和结肠癌细胞中的原发性顺铂耐药性。